Table 1

Inhibitory effects of GFZ (IC₅₀, μM) on the metabolism of statin hydroxy acids in human hepatocytes

Substrate	Pathway	Metabolite	GFZ IC₅₀, μM
SVA	Lactonization	SV	52
	Oxidation	3′-Hydroxy	>200
		Dihydrodiol	>200
	β-oxidation	B1	>200
		B2	>200
		B3	>200
	β-oxidation and glucuronidation	B3-glucuronide	15
AVA	Lactonization	AV	63
	Oxidation	Hydroxy AVA - 1	>200
		Hydroxy AVA - 2	>200
CVA	Lactonization	CV	50
	Oxidation	Hydroxy CVA	49
		Demethylated CVA	>200
RVA	Lactonization	RV	36
	Oxidation	Demethylated RVA	46

Results were obtained following co-incubation, in triplicate for each hepatocyte preparation, of statins (20 μM) and GFZ (10–200 μM) at 37°C for 60 min (SVA, AVA, and CVA) or 120 min (RVA) with human hepatocytes (3 × 10⁶ cells/ml).